Assay Detail
Binding
CHEMBL4821489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus-infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorogenic assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.47 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4530950 | — | — | 1 | 6.46 |
| CHEMBL4862510 | — | — | 1 | 6.23 |
| CHEMBL4872697 | — | — | 1 | 6.14 |
| CHEMBL4852441 | — | — | 1 | 6.14 |
| CHEMBL4874716 | — | — | 1 | 6.07 |
| CHEMBL4861336 | — | — | 1 | 6.05 |
| CHEMBL4874671 | — | — | 1 | 5.71 |
| CHEMBL4472834 | — | — | 1 | 5.59 |
| CHEMBL4877300 | — | — | 1 | 5.49 |
| CHEMBL4877023 | — | — | 1 | 5.42 |
| CHEMBL4847771 | — | — | 1 | 5.38 |
| CHEMBL4877805 | — | — | 1 | 5.36 |
| CHEMBL4796066 | — | — | 1 | 5.26 |
| CHEMBL4858210 | — | — | 1 | 5.18 |
| CHEMBL4859992 | — | — | 1 | 5.08 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 4.80 |
| CHEMBL4473451 | — | — | 1 | 4.56 |
| CHEMBL4545246 | — | — | 1 | 4.53 |
| CHEMBL4438566 | — | — | 1 | 4.44 |
| CHEMBL4846564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4530950 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4862510 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4872697 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4852441 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4874716 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4861336 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4874671 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL4472834 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL4877300 | — | IC50 | = | 3260.0 | nM | 5.49 |
| CHEMBL4877023 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL4847771 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4877805 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL4796066 | — | IC50 | = | 5510.0 | nM | 5.26 |
| CHEMBL4858210 | — | IC50 | = | 6560.0 | nM | 5.18 |
| CHEMBL4859992 | — | IC50 | = | 8270.0 | nM | 5.08 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 15830.0 | nM | 4.80 |
| CHEMBL4473451 | — | IC50 | = | 27570.0 | nM | 4.56 |
| CHEMBL4545246 | — | IC50 | = | 29700.0 | nM | 4.53 |
| CHEMBL4438566 | — | IC50 | = | 36470.0 | nM | 4.44 |
| CHEMBL4846564 | — | IC50 | > | 40000.0 | nM | - |